药品信息:
--------------------------------------------------------------- 详细处方信息以本药内容附件PDF文件(201062718593727.pdf)的“原文Priscribing Information”为准 --------------------------------------------------------------- 部分中文MEEK处方资料(仅供参考)
【药物名称】利培酮 【英文名称】Risperidone 【别名】利培酮 ,维思通 【适应症】急、慢性精神分裂症,各种精神病状态的阳性和阴性症状,也可用于减轻与精神分裂症有关的情感症状。 【功能主治】苯丙异恶唑衍生物,是新一代的抗精神病药。与5~HT2受体和D2受体有很高亲和力, 用于治疗急、慢性精神分裂症以及其它各种精神病性状态的明显的阳性症状(如幻觉、妄想、思维紊乱、敌视、怀疑)和明显的阴性症状(如反应迟钝、情绪淡漠及社交淡漠、少语)。也可减轻与精神分裂症有关的情感症状(如抑郁、负罪感、焦虑)。 【用量用法】初始剂量为1-2mg/日,在3-7日内增加至4-6mg/日,每次加量1-2mg/日,最适剂量为4-6mg/日,可维持治疗或进一步调整。首次发作、老年人及肝肾病患者剂量减半。 【副作用】失眠、焦虑、激越、头痛,以及由于血浆中催乳素浓度增加而引起的溢乳、男子女性型乳房、月经失调、闭经,还会出现体重增加、水肿和肝酶水平升高的现象。偶见体位性低血压、反射性心动过速或高血压以及迟发性运动障碍、恶性症状群、体温失调和癫痫发作。 【药物相互作用】可拮抗左旋多巴和多巴胺激动剂的作用,酰胺咪嗪和肝酶诱导剂可降低本药活性成份的血浆浓度。吩噻嗪、三环抗抑郁药及β-阻断剂可增加本药血药浓度。 【注意事项】(1)对本药过敏者及15岁以下儿童禁用,孕妇、哺乳期不宜服用,服用本品的妇女不应哺乳。(2)患有心血管疾病(如心衰、心肌梗塞、传导异常、脱水、失血及脑血管病变)、帕金森氏综合症或癫痫的病人慎用。 Risperidone Risperidone (pronounced Ris-PEAR-rǐ-dōne) is an atypical antipsychotic used to treat schizophrenia (including adolescent schizophrenia), schizoaffective disorder, the mixed and manic states associated with bipolar disorder, and irritability in children with autism.
Indications and Uses treatment of schizophrenia in adults treatment of schizophrenia in adolescents aged 13-17 years alone or in combination with lithium or valproate, for the short-term treatment of acute manic or mixed episodes associated with Bipolar I Disorder in adults alone in the short-term treatment of acute manic or mixed episodes associated with Bipolar I Disorder in children and adolescents aged 10-17 years treatment of irritability associated with autistic disorder in children and young adults it has also been used as a control drug for people with Tourette's syndrome and other tic disorders.
Risperidone was approved by the United States Food and Drug Administration (FDA) in 1993 for the treatment of schizophrenia.[2]
On August 22, 2007, risperidone was approved as the only drug agent available for treatment of schizophrenia in youth ages 13–17; it was also approved that same day for treatment of bipolar disorder in youth and children ages 10–17, joining lithium. Risperidone contains the functional groups of benzisoxazole and piperidine as part of its molecular structure. In 2003 the FDA approved risperidone for the short-term treatment of the mixed and manic states associated with bipolar disorder. In 2006 the FDA approved risperidone for the treatment of irritability in children and adolescents with autism.[3] The FDA's decision was based in part on a study of autistic children with severe and enduring problems of violent meltdowns, aggression, and self-injury; risperidone is not recommended for autistic children with mild aggression and explosive behavior without an enduring pattern.[4] Like other atypical antipsychotics, risperidone has also been used off-label for the treatment of anxiety disorders, such as obsessive-compulsive disorder; severe, treatment-resistant depression with or without psychotic features; Tourette syndrome; disruptive behavior disorders in children; and eating disorders, among others. In two small studies risperidone was reported to successfully treat the symptoms of phencyclidine (PCP) psychosis due to acute intoxication[5] and chronic use.[6]
A 2009 Cochrane Library review found no evidence from randomized controlled trials that risperidone is effective for the treatment of attention-deficit hyperactivity disorder (ADHD) in people with intellectual disabilities.[7] A multi-year UK study by the Alzheimer's Research Trust suggested that this and other neuroleptic anti-psychotic drugs commonly given to Alzheimer's patients with mild behavioural problems often made their condition worse. The study concluded that:
“ For most patients with AD, withdrawal of neuroleptics had no overall detrimental effect on functional and cognitive status and by some measures improved functional and cognitive status. Neuroleptics may have some value in the maintenance treatment of more severe neuropsychiatric symptoms, but this possibility must be weighed against the unwanted effects of therapy
Side effects Risperidone has been associated with weight gain.[9] Other common side effects include akathisia, sedation, dysphoria, insomnia, sexual dysfunction, low blood pressure, high blood pressure, muscle stiffness, muscle pain, tremors, increased salivation, constipation, and stuffy nose.
Many antipsychotics are known to cause hyperprolactinemia which may lead to hypogonadism-induced osteoporosis, galactorrhoea, gynaecomastia, irregular menstruation and sexual dysfunction. However, risperidone is known to increase prolactin to a greater extent than other atypical antipsychotics. Although lactation is possible in both sexes using other antipsychotic drugs, risperidone is the biggest offender.[10][11] There is a higher association between pituitary neoplasms with use of risperidone and amisulpride than with other antipsychotic agents.[12] It is thought that once risperidone raises prolactin, it may cause prolactinoma, a benign tumor of the pituitary gland. Tumors, in general, are not considered reversible. Medical therapy may help reduce tumor size and restore normal reproduction and pituitary function, however, dopamine agonists are not likely to be prescribed to antipsychotic users, thus, surgery or radiation treatment may be required. This condition may recur if the patient is switched to a different antipsychotic. Risperidone has been known to cause increased thoughts of suicide.[13]
Risperidone can potentially cause tardive dyskinesia (TD),[14] extrapyramidal symptoms (EPS),[14] and neuroleptic malignant syndrome (NMS).[14] Risperidone may also trigger diabetes and more serious conditions of glucose metabolism, including ketoacidosis and hyperosmolar coma.[15]
Pharmacology This drug belongs to a class of antipsychotic drugs known as atypical antipsychotics that have more pronounced serotonin antagonism than dopamine antagonism, but risperidone is unique in this class because it retains dopamine antagonism. It has high affinity for D2 dopaminergic receptors. It has actions at several 5-HT (serotonin) receptor subtypes. These are 5-HT2C, linked to weight gain, 5-HT2A,linked to its antipsychotic action and relief of some of the extrapyramidal side effects (EPS) experienced with the typical neuroleptics. The EPS are a consequence of increased release of dopamine from nigrostriatal neurons in the brain.
It reaches peak plasma levels quickly regardless of whether it is administered as a liquid or pill. Risperidone is metabolised fairly quickly, so the potential for nausea subsides usually in two to three hours. However, the active metabolite, 9-hydroxy-risperidone, which has similar pharmacodynamics to risperidone, lingers in the body for much longer, and has been developed as an antipsychotic in its own right, called paliperidone.
An intramuscular preparation, marketed as Risperdal Consta, can be given once every two weeks. It is slowly released from the injection site. This method of administration may be used on sanctioned patients who are declining, or consenting patients who may have disorganized thinking and cannot remember to take their daily doses.[16] Doses range from 12.5 to 50 mg given as an intramuscular injection once every two weeks.
--------------------------------------------------------------- 详细处方信息以本药内容附件PDF文件(201062718593727.pdf)的“原文Priscribing Information”为准 ---------------------------------------------------------------
2010年6月28日更新 |